Design, Synthesis, and Biological Activity of Novel Octahydro-1Hpyrrolo[3,2-c]pyridine Derivatives as C-C Chemokine Receptor Type 5 (CCR5) Antagonists

doi:10.6023/CJOC201701049

Paper

Design, Synthesis, and Biological Activity of Novel Octahydro-1Hpyrrolo[3,2-c]pyridine Derivatives as C-C Chemokine Receptor Type 5 (CCR5) Antagonists

Published 2017 · Yujie Wang, Upul D. Halambage, Chengchu Zeng

Chinese Journal of Organic Chemistry

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Abstract

A series of novel octahydro-1H-pyrrolo[3,2-c]pyridine derivatives were designed and synthesized as C-C chemokine receptor type 5 (CCR5) antagonists, and their biological activity of anti-human immunodeficiency virus type 1 (HIV-1) is evaluated. A majority of these compounds showed anti-HIV-1 activities. Octahydro-1H-pyrrolo[3,2-c]pyridine derivative 19c exhibited potency against HIV-1 replication less than 1 μmol•L. Function assay was employed and the result showed that there were other drug targets for HIV-1 inhibition besides CCR5. In addition, the preliminary structure-activity relationship (SAR) of these compounds was rationalized by docking studies.

In Vitro Study

Study Snapshot

Novel octahydro-1H-pyrrolo[3,2-c]pyridine derivatives show anti-HIV-1 activities, with potential as CCR5 antagonists and other targets for HIV-1 inhibition.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Design, Synthesis, and Biological Activity of Novel Octahydro-1Hpyrrolo[3,2-c]pyridine Derivatives as C-C Chemokine Receptor Type 5 (CCR5) Antagonists

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